In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B.


:Natural products play a pivotal role in medicine especially in the cancer arena. Many drugs that are currently used in cancer chemotherapy originated from or were inspired by nature. Jerantinine B (JB) is one of seven novel Aspidosperma indole alkaloids isolated from the leaf extract of Tabernaemontana corymbosa. Preliminary antiproliferative assays revealed that JB and JB acetate significantly inhibited growth and colony formation, accompanied by time- and dose-dependent apoptosis induction in human cancer cell lines. JB significantly arrested cells at the G2/M cell cycle phase, potently inhibiting tubulin polymerisation. Polo-like kinase 1 (PLK1; an early trigger for the G2/M transition) was also dose-dependently inhibited by JB (IC50 1.5 µM). Furthermore, JB provoked significant increases in reactive oxygen species (ROS). Annexin V+ cell populations, dose-dependent accumulation of cleaved-PARP and caspase 3/7 activation, and reduced Bcl-2 and Mcl-1 expression confirm apoptosis induction. Preclinical in silico biopharmaceutical assessment of JB calculated rapid absorption and bioavailability >70%. Doses of 8-16 mg/kg JB were predicted to maintain unbound plasma concentrations >GI50 values in mice during efficacy studies. These findings advocate continued development of JB as a potential chemotherapeutic agent.


Cancer Lett


Cancer letters


Qazzaz ME,Raja VJ,Lim KH,Kam TS,Lee JB,Gershkovich P,Bradshaw TD




Has Abstract


2016-01-28 00:00:00














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    journal_title:Cancer letters

    pub_type: 杂志文章,评审


    authors: Ribatti D,Tamma R,Crivellato E

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  • Cells of origin and tumor-initiating cells for nonmelanoma skin cancers.

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    pub_type: 杂志文章,评审


    authors: Thieu K,Ruiz ME,Owens DM

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  • Alterations of cell surface antigens induced by placental isoform of ferritin in human carcinoma cell lines.

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    journal_title:Cancer letters

    pub_type: 杂志文章


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    journal_title:Cancer letters

    pub_type: 杂志文章


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    abstract::Gastric juice ascorbic acid concentrations were examined in black and white patients. Significantly lower concentrations were found in blacks, in the absence of a significant difference in the plasma concentration of vitamin C between races. Blacks had higher prevalence of Helicobacter pylori infection, higher gastric...

    journal_title:Cancer letters

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  • Long non-coding RNAs in glioma progression.

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    journal_title:Cancer letters

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    authors: Xi J,Sun Q,Ma L,Kang J

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    authors: Chen YL,Chang MC,Chiang YC,Lin HW,Sun NY,Chen CA,Sun WZ,Cheng WF

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  • BCLB, methylated in hepatocellular carcinoma, is a starvation stress sensor that induces apoptosis and autophagy through the AMPK-mTOR signaling cascade.

    abstract::Epigenetic disruption of tumor suppressor genes (TSGs), particularly DNA methylation, plays a key role in hepatocellular carcinoma (HCC) pathogenesis. Through methylome study, we identified BCLB as a methylated gene in HCC. BCLB was methylated in all tumor cell lines with silenced or reduced expression. BCLB was furth...

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    authors: Liu X,Hu X,Kuang Y,Yan P,Li L,Li C,Tao Q,Cai X

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    journal_title:Cancer letters

    pub_type: 杂志文章,评审


    authors: Li L,Wang H

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    journal_title:Cancer letters

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    journal_title:Cancer letters

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    pub_type: 杂志文章


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    authors: Takahashi T,Ogawa H,Izumi K,Uehara H

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    authors: Xu Z,Wang Z,Jia X,Wang L,Chen Z,Wang S,Wang M,Zhang J,Wu M

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    journal_title:Cancer letters

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    authors: Rivedal E

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    journal_title:Cancer letters

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    journal_title:Cancer letters

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    journal_title:Cancer letters

    pub_type: 杂志文章


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    journal_title:Cancer letters

    pub_type: 杂志文章


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    journal_title:Cancer letters

    pub_type: 杂志文章


    authors: Ozawa F,Friess H,Kleeff J,Xu ZW,Zimmermann A,Sheikh MS,Büchler MW

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    journal_title:Cancer letters

    pub_type: 杂志文章


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